反应详情

温度

120 °C

tert-Butyl 4-((3-amino-5-bromobenzyloxy)methyl)-4-phenylpiperidine-1-carboxylate (220.0 mg, 0.46 mmol), 4-cyanophenylboronic acid (273.0 mg, 1.86 mmol), and tetrakis(triphenylphosphine) palladium(0) (71.7 mg, 0.046 mmol) were combined in dry tetrahydrofuran (5 mL) in a microwave tube and sealed. The mixture was flushed with nitrogen. To this was added potassium hydroxide (1 N in water, 1.4 mL, 1.4 mmol). The mixture was heated at 120° C. for 1 h via microwave. After cooling to room temperature, the reaction mixture was concentrated and purified by flash chromatography on silica gel (25% ethyl acetate/hexanes) to afford 140.0 mg (61%). LC/MS (HPLC method 3): tR=2.85 min, 498.24 (MH)+.

1. customsealed
2. customThe mixture was flushed with nitrogen
3. temperatureAfter cooling to room temperature
4. concentrationthe reaction mixture was concentrated
5. custompurified by flash chromatography on silica gel (25% ethyl acetate/hexanes)
6. customto afford 140.0 mg (61%)